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1. 发明授权

US08097610B2 Derivative having PPAR agonistic activity 有权
标题翻译：具有PPAR激动活性的衍生物
公开(公告)号：US08097610B2
公开(公告)日：2012-01-17
申请号：US11990977
申请日：2006-08-24
申请人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takafumi Ohara , Terukazu Kato
发明人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takafumi Ohara , Terukazu Kato
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/4535 , C07D401/04 , C07D413/14 , C07D417/04
CPC分类号： C07D211/22 , C07D211/58 , C07D241/04 , C07D241/44 , C07D277/82 , C07D401/04 , C07D403/04 , C07D413/14 , C07D417/04 , C07D417/12
摘要： A compound of the formula (I): or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）的化合物或其药学上可接受的盐。

2. 发明申请

US20110294813A1 OXAZOLIDINONE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 审中-公开
标题翻译：在11BETA-羟基脱氢酶脱氢酶1型上具有抑制活性的奥沙利酮衍生物
公开(公告)号：US20110294813A1
公开(公告)日：2011-12-01
申请号：US13173819
申请日：2011-06-30
申请人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
发明人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
IPC分类号： A61K31/4439 , C07D263/24 , A61P3/10 , A61K31/454 , A61K31/5377 , A61K31/496 , C07D413/12 , A61K31/421
CPC分类号： C07D263/20 , A61K31/421 , A61K31/422 , A61K31/4412 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D413/12
摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(═O)— or —NR3S(═O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.
摘要翻译：公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。由下式表示的化合物：其药学上可接受的盐或其溶剂化物，其中R 1是任选取代的环烷基，任选取代的环烷基烷基，任选取代的杂环或任选取代的杂环烷基，X是-O-，-NR 3 - ， - NR 3 C（= O） - 或-NR 3 S（= O）2 - ，R 2是任选取代的芳基，任选取代的芳基烷基，任选取代的杂芳基或任选取代的杂芳基烷基，R 3是氢或任选取代的烷基。

3. 发明申请

US20100234363A1 HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 DATA-HYDROXYSTEROID DEHYDROGENASE 审中-公开
标题翻译：具有I型11数据羟基脱氢酶抑制活性的杂环衍生物
公开(公告)号：US20100234363A1
公开(公告)日：2010-09-16
申请号：US12679159
申请日：2008-09-17
申请人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
发明人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
IPC分类号： A61K31/5415 , C07D279/08 , A61P3/10 , C07D265/24 , A61K31/536
CPC分类号： C07D279/06 , C07D265/24 , C07D279/08 , C07D417/04 , C07D417/12
摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.
摘要翻译：公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中X为O或S，虚线和波浪线表示存在或不存在键，（i）当虚线表示键的存在，波浪线表示不存在键，R2和R3各自独立地为氢，卤素，氰基，羟基，羧基，任选取代的烷基，任选取代的烯基，任选取代的炔基等，（ii）当虚线表示不存在键，波浪线表示键的存在，R 1和R 4各自独立地为氢，卤素等，R 2和R 3各自独立地为氢，卤素，氰基，羟基，羧基，任选地取代的烷基，任选取代的烯基，任选取代的炔基等，R 5和R 6各自独立地为氢，任选取代的烷基，任选取代的烯基，任选取代的炔基等。

4. 发明申请

US20100113448A1 OXAZOLIDINONE DERIVATIVE HAVING INHIBITORY ACTIVITY ON 11BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 失效
标题翻译：在11BETA-羟基脱氢酶脱氢酶1型上具有抑制活性的奥沙利酮衍生物
公开(公告)号：US20100113448A1
公开(公告)日：2010-05-06
申请号：US12594093
申请日：2008-03-27
申请人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
发明人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
IPC分类号： A61K31/421 , C07D413/12 , C07D263/24 , A61P3/10 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K31/496
CPC分类号： C07D263/20 , A61K31/421 , A61K31/422 , A61K31/4412 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D413/12
摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(═O)— or —NR3S(═O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.
摘要翻译：公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中R 1是任选取代的环烷基，任选取代的环烷基烷基，任选取代的杂环或任选取代的杂环烷基，X是-O-，-NR 3 - ， - NR 3 C（= O） - 或-NR 3 S（= O）2 - ，R 2是任选取代的芳基，任选取代的芳基烷基，任选取代的杂芳基或任选取代的杂芳基烷基，R 3是氢或任选取代的烷基。

5. 发明授权

US07998992B2 Oxazolidinone derivative having inhibitory activity on 11β-hydroxysteroid dehydrogenase type 1 失效
标题翻译：具有抑制活性的恶唑烷酮衍生物，其为11＆bgr-羟基类固醇脱氢酶1型
公开(公告)号：US07998992B2
公开(公告)日：2011-08-16
申请号：US12594093
申请日：2008-03-27
申请人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
发明人： Akiko Itai , Susumu Muto , Ryuko Tokuyama , Hiroshi Fukasawa , Takeshi Yanase
IPC分类号： A01N43/76 , A01N43/36 , A61K31/42 , A61K31/535 , A61K31/40 , C07D263/00
CPC分类号： C07D263/20 , A61K31/421 , A61K31/422 , A61K31/4412 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , C07D413/12
摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocycle or optionally substituted heterocyclealkyl, X is —O—, —NR3—, —NR3C(═O)— or —NR3S(═O)2—, R2 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, R3 is hydrogen or optionally substituted alkyl.
摘要翻译：公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。由下式表示的化合物：其药学上可接受的盐或其溶剂化物，其中R 1是任选取代的环烷基，任选取代的环烷基烷基，任选取代的杂环或任选取代的杂环烷基，X是-O-，-NR 3 - ， - NR 3 C（= O） - 或-NR 3 S（= O）2 - ，R 2是任选取代的芳基，任选取代的芳基烷基，任选取代的杂芳基或任选取代的杂芳基烷基，R 3是氢或任选取代的烷基。

6. 发明申请

US20090286974A1 Derivative having ppar agonistic activity 有权
标题翻译：衍生物具有ppar激动活性
公开(公告)号：US20090286974A1
公开(公告)日：2009-11-19
申请号：US11990977
申请日：2006-08-24
申请人： Akiko Itai , Susumu Muto , RYuko Tokuyama , Hiroshi Fukasawa , Takafumi Ohara , Terukazu Kato
发明人： Akiko Itai , Susumu Muto , RYuko Tokuyama , Hiroshi Fukasawa , Takafumi Ohara , Terukazu Kato
IPC分类号： C07D417/04 , C07D403/04
CPC分类号： C07D211/22 , C07D211/58 , C07D241/04 , C07D241/44 , C07D277/82 , C07D401/04 , C07D403/04 , C07D413/14 , C07D417/04 , C07D417/12
摘要： A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein Ring Q is optionally substituted monocyclic aryl, optionally substituted monocyclic heteroaryl, optionally substituted fused aryl or optionally substituted fused heteroaryl, Y1 is a bond or —NR6— or the like, Ring A is optionally substituted nonaromatic heterocyclediyl, a group of the formula: -Y2Z1- is a group of the formula: R7 are each independently hydrogen, optionally substituted lower alkyl or the like, R8 and R9 are each independently hydrogen or optionally substituted lower alkyl, n is an integer between 1 and 3, Z1 is a bond, —O—, —S— or —NR9—, Ring B is optionally substituted aromatic carbocyclediyl or optionally substituted aromatic heterocyclediyl, Y3 is a bond, optionally substituted lower alkylene optionally intervened by —O—, optionally substituted lower alkenylene or the like, and Z2 is COOR3 or the like.
摘要翻译：式（I）的化合物：其药学上可接受的盐或溶剂化物，其中环Q是任选取代的单环芳基，任选取代的单环杂芳基，任选取代的稠合芳基或任选取代的稠合杂芳基，Y1是键或-NR 6 - 或环A是任选取代的非芳族杂环二基，下式基团：-Y 2 Z 1 - 是下式的基团：R 7各自独立地为氢，任选取代的低级烷基等，R 8和R 9各自独立地为氢或任选地取代的低级烷基，n是1和3之间的整数，Z 1是键，-O-，-S-或-NR 9 - ，环B是任选取代的芳族碳环二基或任选取代的芳族杂环二基，Y 3是一个键，任选地被-O-，任选取代的低级亚烯基等所介导的低级亚烷基，Z 2是COOR 3等。

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